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. 1995 Apr 7;268(5207):80-3.
doi: 10.1126/science.7701344.

E5531, a pure endotoxin antagonist of high potency

W J Christ  1 , O Asano, A L Robidoux, M Perez, Y Wang, G R Dubuc, W E Gavin, L D Hawkins, P D McGuinness, M A Mullarkey, et al.
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"VSports手机版" E5531, a pure endotoxin antagonist of high potency

W J Christ et al. Science. .

Abstract

Shock due to Gram-negative bacterial sepsis is a consequence of acute inflammatory response to lipopolysaccharide (LPS) or endotoxin released from bacteria. LPS is a major constituent of the outer membrane of Gram-negative bacteria, and its terminal disaccharide phospholipid (lipid A) portion contains the key structural features responsible for toxic activity. Based on the proposed structure of nontoxic Rhodobacter capsulatus lipid A, a fully stabilized endotoxin antagonist E5531 has been synthesized. In vitro, E5531 demonstrated potent antagonism of LPS-mediated cellular activation in a variety of systems. In vivo, E5531 protected mice from LPS-induced lethality and, in cooperation with an antibiotic, protected mice from a lethal infection of viable Escherichia coli VSports手机版. .

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